138382-23-7
Chemical Structure
L 366509
- CAS No.: 138382-23-7
- Formula:C25H33NO5S
- Molecular Weight:459.60
IUPAC Name: 2-((1S,2S,4R)-2-hydroxy-7,7-dimethyl-1-((spiro[indene-1,4'-piperidin]-1'-ylsulfonyl)methyl)bicyclo[2.2.1]heptan-2-yl)acetic acid
InChIKey: XKVDTEPESVJNPJ-NGXZDTIWSA-N
SMILES: O=S(N(CC1)CCC21C3=CC=CC=C3C=C2)(C[C@]4(C5(C)C)CC[C@@H]5C[C@@]4(CC(O)=O)O)=O
Biological Activity: L 366509 is a spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist. Modifications led to a new series of o-tolylpiperazine (TP) camphorsulfonamides, exhibiting high affinity for OT receptors and selectivity over arginine vasopressin receptors. Notably, compound 7 (L-368,899) showed excellent OT receptor affinity, potency in inhibiting OT-stimulated uterine contractions, good aqueous solubility, and oral bioavailability in multiple species. Compound 7 has entered clinical testing as an oral and intravenous tocolytic agent. Molecular modeling suggests the TP camphorsulfonamide structure mimics the D-AA2-Ile3 dipeptide, crucial in potent OT antagonists[1].
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L 366509 | L 366509 is a spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist. Modifications led to a new series of o-tolylpiperazine (TP) camphorsulfonamides, exhibiting high affinity for OT receptors and selectivity over arginine vasopressin receptors. Notably, compound 7 (L-368,899) showed excellent OT receptor affinity, potency in inhibiting OT-stimulated uterine contractions, good aqueous solubility, and oral bioavailability in multiple species. Compound 7 has entered clinical testing as an oral and intravenous tocolytic agent. Molecular modeling suggests the TP camphorsulfonamide structure mimics the D-AA2-Ile3 dipeptide, crucial in potent OT antagonists. | |||||||||||||||||||||
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